JP2025508702A - キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 - Google Patents
キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 Download PDFInfo
- Publication number
- JP2025508702A JP2025508702A JP2024547690A JP2024547690A JP2025508702A JP 2025508702 A JP2025508702 A JP 2025508702A JP 2024547690 A JP2024547690 A JP 2024547690A JP 2024547690 A JP2024547690 A JP 2024547690A JP 2025508702 A JP2025508702 A JP 2025508702A
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- Prior art keywords
- cancer
- fluoro
- amino
- compound
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263310915P | 2022-02-16 | 2022-02-16 | |
| US63/310,915 | 2022-02-16 | ||
| PCT/US2023/062687 WO2023159086A1 (en) | 2022-02-16 | 2023-02-15 | Quinazoline compounds and use thereof as inhibtors of mutant kras proteins |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2025508702A true JP2025508702A (ja) | 2025-04-10 |
| JP2025508702A5 JP2025508702A5 (enExample) | 2026-02-25 |
Family
ID=85685573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024547690A Pending JP2025508702A (ja) | 2022-02-16 | 2023-02-15 | キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20250163064A1 (enExample) |
| EP (1) | EP4479401A1 (enExample) |
| JP (1) | JP2025508702A (enExample) |
| CN (1) | CN118974055A (enExample) |
| AU (1) | AU2023222076A1 (enExample) |
| CA (1) | CA3251001A1 (enExample) |
| MX (1) | MX2024010045A (enExample) |
| WO (1) | WO2023159086A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN119569702A (zh) | 2018-04-04 | 2025-03-07 | 阿尔维纳斯运营股份有限公司 | 蛋白水解调节剂及相关使用方法 |
| JP2025541682A (ja) | 2022-11-21 | 2025-12-23 | ツリーライン バイオサイエンシズ インコーポレイテッド | スピロ環式ジヒドロピランピリミジンＫＲａｓ阻害剤 |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| CN121712509A (zh) | 2023-05-04 | 2026-03-20 | 锐新医药公司 | 用于ras相关疾病或病症的组合疗法 |
| TW202504599A (zh) | 2023-06-30 | 2025-02-01 | 美商必治妥美雅史谷比公司 | Kras抑制劑 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202515570A (zh) | 2023-08-17 | 2025-04-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并嘧啶ｋｒａｓ抑制劑 |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| AU2024344161A1 (en) | 2023-09-21 | 2026-03-26 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| AU2024354737A1 (en) | 2023-10-06 | 2026-04-16 | Amgen Inc. | Combination therapy for cancer treatment |
| AU2024358992A1 (en) | 2023-10-09 | 2026-04-23 | Incyte Corporation | Combination comprising a kras g12d inhibitor and an egfr inhibitor for use in the treatment of cancer |
| WO2025080593A1 (en) | 2023-10-09 | 2025-04-17 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| IL327306A (en) | 2023-10-12 | 2026-05-01 | Revolution Medicines Inc | Macrocyclic RAS inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090333A1 (en) | 2024-10-23 | 2026-04-30 | Incyte Corporation | Combination using a kras g12d inhibitor and chemotherapy combinations as well as their use in the treatment of cancer |
| WO2026090323A1 (en) | 2024-10-23 | 2026-04-30 | Incyte Corporation | Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor and its use in the treatment of cancer |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10822312B2 (en) * | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| PH12019500056B1 (en) | 2016-07-12 | 2024-01-31 | Revolution Medicines Inc | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| BR112019015075A2 (pt) | 2017-01-23 | 2020-03-10 | Revolution Medicines, Inc. | Compostos bicíclicos como inibidores de shp2 alostéricos |
| SG11201906412SA (en) | 2017-01-23 | 2019-08-27 | Revolution Medicines Inc | Pyridine compounds as allosteric shp2 inhibitors |
| ES2905676T3 (es) | 2017-05-22 | 2022-04-11 | Amgen Inc | Inhibidores de KRAS G12C y métodos para su uso |
| CN111051306B (zh) | 2017-09-08 | 2023-01-03 | 美国安进公司 | Kras g12c的抑制剂及其使用方法 |
| SG11202002941WA (en) | 2017-10-12 | 2020-04-29 | Revolution Medicines Inc | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| CA3123227A1 (en) | 2018-12-20 | 2020-06-25 | Amgen Inc. | Heteroaryl amides useful as kif18a inhibitors |
| PE20211475A1 (es) | 2018-12-20 | 2021-08-05 | Amgen Inc | Inhibidores de kif18a |
| WO2020132651A1 (en) | 2018-12-20 | 2020-06-25 | Amgen Inc. | Kif18a inhibitors |
| MX2021007157A (es) | 2018-12-20 | 2021-08-16 | Amgen Inc | Heteroarilamidas utiles como inhibidores de kif18a. |
| EP4203952A4 (en) * | 2020-08-28 | 2024-12-11 | Kumquat Biosciences Inc. | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| CN113999226B (zh) * | 2020-12-22 | 2023-01-06 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| JP2024506329A (ja) * | 2021-02-09 | 2024-02-13 | カムクワット バイオサイエンシーズ インコーポレイテッド | 複素環式化合物およびその使用 |
| JP2024508755A (ja) * | 2021-02-16 | 2024-02-28 | セラス， インコーポレイテッド | Ｋｒａｓを阻害するための組成物及び方法 |
| WO2022184178A1 (en) * | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| MX2023014786A (es) * | 2021-06-10 | 2024-01-11 | Redx Pharma Plc | Derivados quinazolina utiles como inhibidores de ras. |
-
2023
- 2023-02-15 MX MX2024010045A patent/MX2024010045A/es unknown
- 2023-02-15 CN CN202380032897.3A patent/CN118974055A/zh active Pending
- 2023-02-15 US US18/838,954 patent/US20250163064A1/en active Pending
- 2023-02-15 WO PCT/US2023/062687 patent/WO2023159086A1/en not_active Ceased
- 2023-02-15 AU AU2023222076A patent/AU2023222076A1/en active Pending
- 2023-02-15 EP EP23711641.3A patent/EP4479401A1/en active Pending
- 2023-02-15 JP JP2024547690A patent/JP2025508702A/ja active Pending
- 2023-02-15 CA CA3251001A patent/CA3251001A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2023159086A1 (en) | 2023-08-24 |
| EP4479401A1 (en) | 2024-12-25 |
| MX2024010045A (es) | 2024-08-26 |
| US20250163064A1 (en) | 2025-05-22 |
| AU2023222076A1 (en) | 2024-08-15 |
| CN118974055A (zh) | 2024-11-15 |
| CA3251001A1 (en) | 2023-08-24 |
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| A521 | Request for written amendment filed |
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